Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective alpha-sulfone hydroxamates.

Stephen A Kolodziej,Susan L Hockerman,Terri L Boehm,Jeffery N Carroll,Gary A DeCrescenzo,Joseph J McDonald,Debbie A Mischke,Grace E Munie,Theresa R Fletcher,Joseph G Rico,Nathan W Stehle,Craig Swearingen,Daniel P Becker

Bioorganic & medicinal chemistry letters（2010）

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摘要

A series of phenyl piperidine alpha-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13, are dual-sparing of MMP-1 and MMP-14 (MT1-MMP) and exhibit oral bioavailability in rats.

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